This invention relates to novel indolobenzazepine derivatives, which are useful as either minor tranquilizers (anxiolytics) or as major tranquilizers (antipsychotics), or as both.
Iminodibenzyl can be named according to the IUPAC 1957 Rules 10,11-dihydro-5H-dibenz[b,f]azepine. This compound was described by Thiele and Holzinger as early as 1899 [Ann. Chem 305, page 100]. These authors also reported nitrosation of the iminodibenzyl and formation of N-nitroso iminodibenzyl [ibid, 102]. Certain benzazepino-pyrido-indole derivatives have been described in U.S. Pat. Nos. 3,373,153; 3,373,154; 3,373,168; and 3,457,271. The last named patent describes 11-(lower alkyl)hexahydro-1- benzazepino[3,2,1-h,i]pyrido[4,3-b]indoles, which are intermediates to 11-(lower alkyl)octahydrobenzazepino[ 3,2,1-h,i]pyrido[4,3-b]indoles. The octahydro compounds are antidepressants. These compounds can be represented by the generic formula (1) ##SPC1##
Where ' is a straight or branched-chain alkyl having 1-7 carbon atoms.
South African patent No. 680,169 discloses a group of benzazepino-pyrido-indole derivatives of formula (2), which possess a "marked depressant activity on the central nervous system and are useful as sedatives and tranquilizers." ##SPC2##
R" is hydrogen or a straight chain alkyl group of no more than 4 carbon atoms.
The South African patent does not describe more closely the type of depressant activity of these novel compounds.
General, nonselective central nervous system depressants are one class of drugs well recognized in the art [L.S. Goodman and A. Gilman (Eds.), The Pharmacologic Basis of Therapeutics, 4th Ed., The Macmillan Co., N.Y., 1970]. Included in this category are anesthetic gases and vapors, aliphatic alcohols and the barbiturates and related sedativehypnotic drugs. These agents share the common property of depressing all excitable tissue.
Also well recognized in the art is another class of depressant drugs known as selective central system depressants [ibid, page 40]. In contrast to the nonselective depressants, these drugs selectively affect particular central nervous system functions. Included in this category are major tranquilizers such as the phenothiazines, and minor tranquilizers exemplified by the benzodiazepines. The former, also known as antipsychotics, are used mainly in schizophrenia and other psychoses, while the latter, also known as anxiolytics, are effective in behavioral states characterized by anxiety and tension.
Most commonly used drugs, whether minor tranquilizers or major tranquilizers have undesirable side effects, including ataxia and physical dependence. There often also are undesirable pharmacological side effects which limit their usefulness, such as jaundice, parkinsonism, dyskinesia, faintness, palpitation, dry mouth, and so on.
There is, therefore, a need in the art for additional psychotherapeutic agents which would have fewer side effects than those used today and which would be effective for the treatment of either neuroses or psychoses.